Design and optimization of oleanolic/ursolic acid-loaded nanoplatforms for ocular anti-inflammatory applications

This work reports the design and development by solvent displacement of poly(lactic-co-glycolic) acid nanoparticles for the ocular delivery of pentacyclic triterpenes oleanolic/ursolic acids. The combined influence of 5-level, 3-factor variables on the physicochemical properties of the nanoparticles was studied by central rotatable composite design 23 + star. After optimization, nanoparticles < 225 nm sized with homogeneous distribution, negatively charged surface (∼−27 mV), high entrapment efficiency (∼ 77%) and good stability were obtained. Drug release and corneal permeation studies were performed. Furthermore, in vitro and in vivo studies confirmed no sign of irritation or toxicity and successful ocular anti-inflammatory efficacy.185